Cocaine is a useful therapeutic used in many different products such as nasal spray. The first total synthesis of cocaine was published in 1923 by Wilstätter, Wolfes and Mader. The procedure was modified and significantly improved in the works of Findlay and then Casale. It involved preparation of racemic 2-carbomethoxytropinone, resolution of the racemate and reduction of the resulting enantiomerically pure 2-carbomethoxytropinone by sodium amalgam to obtain methyl ecgonine. Benzoylation of the latter afforded cocaine. To the best of our knowledge this is still the most convenient and practical procedure reported in the literature. However, this synthesis remains laborious, time consuming, requires distillation of large quantities of organic solvents and involves tedious separation of enantiomers.
Novel synthetic approaches to enantiomerically pure cocaine although elegant, can hardly be used for a large scale production as they involve complicated multistep synthesis and use rather expensive chemicals.